Intermediate for making 3-oxo-4-aza-androst-1-ene 17β-ketones

Abstract

Described is a new intermediate and new process for preparing 3-oxo-4-aza-androst-1-ene 17β-ketones. The process involves converting the corresponding 17β-alkyl carboxylate to the N-methoxy-N-methyl carboxamide and reacting this with an appropriate Grignard reagent to form the desired ketone. The reaction can be conducted in "one pot", thus eliminating isolation of intermediates and avoiding the use of less stable intermediates, e.g., acid chlorides, acyl imidazolides and the like. The intermediate has the formula: ##STR1## wherein R 1 is hydrogen.

What is claimed is: 
     
       1. A method for preparing a compound of the formula: ##STR10## wherein R 1  is hydrogen; which process comprises reacting a compound of the formula ##STR11## wherein R 2  is C 1  -C 4  alkyl; with N,O-dimethylhydroxylamine and RMgX in a dry inert organic solvent, in dry atmosphere, at a temperature of 0° to 25° C., for a sufficient time to form the amide II. 
     
     
       2. A compound of the formula ##STR12## wherein R 1  is hydrogen.